文章：

NF-κB抑制剂对抗癌药物的增敏作用

Nuclear factor-κB inhibitors as sensitizers to anticancer drugs

原文发布日期：2005-04-01

DOI: 10.1038/nrc1588

类型: Review Article

开放获取: 否

要点：

1. Many anticancer agents induce nuclear factor-κB (NF-κB) nuclear translocation and activation of its target genes, which impinge on cellular resistance to anticancer agents.
2. Many malignant tumours display constitutive NF-κB activation that allows malignant cells to escape apoptosis.
3. NF-κB inhibition prevents tumour resistance to chemotherapeutic agents, so development of NF-κB inhibitors could increase the efficacy of many anticancer agents.
4. Several NF-κB inhibitors, such as proteasome inhibitors, BAY 11-7085, BAY 11-7082, soy isoflavone genistein, parthenolide, CHS 828, flavopiridol and gliotoxin, enhance the cytotoxic effect of anticancer agents.
5. It has also been demonstrated that steroids and non-steroidal anti-inflammatory drugs, such as cyclooxygenase-2 inhibitors, block NF-κB activation.

要点翻译：

1. 许多抗癌药物会诱导核因子κB（NF-κB）发生核转位并激活其靶基因，这会影响细胞对抗癌药物的耐药性。
2. 许多恶性肿瘤表现出持续活化的NF-κB，使得恶性细胞能够逃避凋亡。
3. 抑制NF-κB可阻止肿瘤对化疗药物的耐药，因此开发NF-κB抑制剂有望提高多种抗癌药物的疗效。
4. 已有多种NF-κB抑制剂（如蛋白酶体抑制剂、BAY 11-7085、BAY 11-7082、大豆异黄酮染料木素、小白菊内酯、CHS 828、夫拉平度及胶霉毒素）被证实能增强抗癌药物的细胞毒性作用。
5. 研究还表明，甾体类和非甾体类抗炎药（如环氧合酶-2抑制剂）也可阻断NF-κB的活化。

英文摘要：

The cytotoxicity of chemotherapeutic agents is attributed to apoptosis. Acquired resistance to the effects of chemotherapy has emerged as a significant impediment to effective cancer therapy. One feature that cytotoxic treatments of cancer have in common is their activation of the transcription factor nuclear factor-κB (NF-κB), which regulates cell survival. NF-κB activation suppresses the apoptotic potential of chemotherapeutic agents and contributes to resistance. What evidence is there that inhibitors of NF-κB might promote apoptosis in cancer cells and can NF-κB inhibitors be used to overcome resistance to chemotherapeutic agents?

摘要翻译： 

化疗药物的细胞毒性归因于细胞凋亡。然而，对化疗效应的获得性耐药已成为有效癌症治疗的一大障碍。各种细胞毒治疗的一个共同点是它们都能激活转录因子核因子-κB（NF-κB），后者调控细胞存活。NF-κB的激活会抑制化疗药物诱导凋亡的能力，从而导致耐药。那么，有哪些证据表明NF-κB抑制剂可能促进癌细胞凋亡？NF-κB抑制剂又能否用于克服对化疗药物的耐药？

原文链接：

Nuclear factor-κB inhibitors as sensitizers to anticancer drugs